Anhydrous Melatonin Bulk Solution for Parenteral Stability
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current methods fail to provide a stable and convenient pharmaceutical solution with high concentrations of melatonin suitable for parenteral administration, as melatonin is poorly soluble in water, light-sensitive, and unstable in aqueous solutions, leading to instability and low bioavailability when used intravenously.
Innovation Solution
A substantially water-free bulk solution of melatonin is developed, dissolved in a carrier mixture of ethanol and polyethoxylated derivatives at an optimal ratio, achieving solubility up to 10% concentration, which is stable and suitable for intravenous administration without preservatives, ensuring chemical and physical stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If melatonin is dissolved in water to create an injectable solution, then the solution can be administered intravenously, but the solubility is poor and stability is low leading to degradation
Solution Approach 1:
The patent changes the chemical parameters of the solvent system by replacing water with a non-aqueous carrier mixture comprising ethanol and polyethoxylated derivative. This parameter change enables high solubility of melatonin (达到10%以上) while maintaining stability during storage and administration, resolving the contradiction between solubility and stability in aqueous solutions
Solution Approach 2:
The patent uses a composite carrier system consisting of ethanol and polyethoxylated derivative in specific ratios. This composite material provides synergistic effects: ethanol enhances solubility while the polyethoxylated derivative stabilizes the melatonin molecule, together achieving both high solubility and long-term stability that neither component could achieve alone
2Productivity
If the concentration of melatonin is increased to reduce administration volume, then the efficiency of treatment improves, but the solubility limit in water is exceeded causing precipitation
Solution Approach 1:
By changing from aqueous to non-aqueous carrier system, the patent dramatically expands the solubility parameter, enabling concentrations of 10% or higher. This allows high treatment efficiency through reduced administration volume without precipitation, as the non-aqueous carriers can dissolve much higher concentrations of melatonin than water
3Reliability
If preservatives are added to prevent degradation during storage, then the stability improves, but the complexity of the formulation increases and potential side effects arise
Solution Approach 1:
The non-aqueous carrier system itself provides the stabilizing function that would otherwise require separate preservatives. The ethanol and polyethoxylated derivative create an environment that inherently prevents microbial growth and chemical degradation, making the formulation self-stabilizing and eliminating the need for additional preservative agents
Solution Approach 2:
The patent extracts and eliminates preservatives from the formulation by using a carrier system that provides inherent stability. The non-aqueous environment naturally prevents degradation without requiring additional chemical agents, simplifying the formulation while maintaining or improving stability
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The solution provides a stable and highly concentrated melatonin bulk solution that can be conveniently diluted for intravenous use, improving bioavailability and stability, addressing the limitations of existing formulations by maintaining solubility and stability during storage and administration.
Implementation Method 1
melatonin is dissolved in a substantially water-free carrier mixture of ethanol and polyethoxylated derivative admixed in an optimal ratio to almost double melatonin solubility profile
Data Source
Figure 1
Figure 2
AI summary
The present invention relates to a concentrated melatonin solution, wherein melatonin is present in a quantity of 10.0 % or higher in a substantially water-free carrier mixture of ethanol and a polyethoxylated derivative. The concentrated solution, free of preserving agents, is suitable to prepare injectable sterile compositions for parenteral administration, or formulations for topical or oral administration. The invention also encompasses a method for the preparation of the concentrated solution, as well as the possible benefits of the intravenous infusion of high levels of melatonin as adjuvant therapy in Ebola or Dengue hemorrhagic fever (DHF) or as an anti-oxidant/anti-aging treatment.